8W9B
CryoEM structure of human PI3K-alpha (P85/P110-H1047R) with QR-8557 binding at an allosteric site
Summary for 8W9B
Entry DOI | 10.2210/pdb8w9b/pdb |
EMDB information | 37363 |
Descriptor | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha, 1-[(1S)-1-(5-fluoranyl-3-methyl-1-benzofuran-2-yl)-2-methyl-propyl]-3-(1-oxidanylidene-2,3-dihydroisoindol-5-yl)urea (3 entities in total) |
Functional Keywords | pi3k-alpha, lipid kinase, allosteric inhibition, oncoprotein |
Biological source | Homo sapiens (human) More |
Total number of polymer chains | 2 |
Total formula weight | 158293.14 |
Authors | |
Primary citation | Huang, X.,Wang, K.,Han, J.,Chen, X.,Wang, Z.,Wu, T.,Yu, B.,Zhao, F.,Wang, X.,Li, H.,Xie, Z.,Zhu, X.,Zhong, W.,Ren, X. Cryo-EM structures reveal two allosteric inhibition modes of PI3K alpha H1047R involving a re-shaping of the activation loop. Structure, 2024 Cited by PubMed: 38582077DOI: 10.1016/j.str.2024.03.007 PDB entries with the same primary citation |
Experimental method | ELECTRON MICROSCOPY (3 Å) |
Structure validation
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